- The Reaction of Phosphorus Decasulfide with some Hydrazides and their Hydrazones: New Route for Construction of Four-membered, Five-membered, and Six-membered Phosphorus Heterocycles
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Reaction of some selected benzoic acid hydrazides 1a–c with phosphorus decasulfide P4S10 in dry pyridine afforded some novel pyridine solvate of 1,3,4,2-thiadiazaphospholes 2a–c. Similarly, treatment of their corresponding hydrazones 3a–c toward phosphorus decasulfide under the same reaction conditions gave the corresponding thio-analog 4 and 1,3,2-benzoxazaphosphinine and benzodiazaphosphinine pyridine solvates 5a,b, respectively. Treatment of (thio)semicarbazides and their corresponding (thio)semicarbazones with phosphorus decasulfide in dry pyridine yielded the novel 1,2,4,3-triazaphospholidines 6a,b, and 1,3,2-diazaphosphetidines 8a,b, respectively. Moreover, cyclization of (thio)carbohydrazides and their mono-(thio)carbohydrazones with phosphorus decasulfide produced 1,2,4,3-triazaphospholidines 9a,b and 11a,b, respectively. The structures of these products were confirmed from analytical and spectral data.
- Abdel-Kariem, Somaia M.,Ali, Tarik E.
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Read Online
- Synthesis, antibacterial activities and molecular docking study of thiouracil derivatives containing oxadiazole moiety
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A series of novel thiouracil derivatives 9 containing an oxadiazole moiety have been synthesized by structural modification of a lead SecA inhibitor, 2. These compounds have been evaluated for their antibacterial activities against Bacillus amyloliquefaciens, Staphylococcus aureus and Bacillus subtilis. Among them, compounds 9g and 9n exhibited promising antibacterial activities against the tested strains. Compound 9g was also tested for its inhibitory activities against SecA ATPase, and the IC50 value of compound 9g was 19.9 μg/mL, lower than that of compound 2 (20.8 μg/mL). Molecular docking work indicates that compound 9g likely occupies the pocket formed by SecA IRA2 and NBD domain.
- Cui, Peng-Lei,Zhang, Di,Guo, Xiu-Min,Ji, Shu-Jing,Jiang, Qing-Mei
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supporting information
p. 1754 - 1762
(2021/04/09)
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- Synthesis and anticonvulsant evaluation of indoline derivatives of functionalized aryloxadiazole amine and benzothiazole acetamide
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A series of N-(substituted benzothiazole-2-yl)-2-(2,3-dioxoindolin-1-yl)acetamide (4a-i) and substituted-[3-((5-phenyl-1,3,4-oxadiazole-2-yl)imino)indolene-2-one] (5a-f) were designed, synthesized fulfilling the structural requirement of pharmacophore and evaluated for anticonvulsant activities using maximal electroshock test (MES), subcutaneous pentylenetetrazole (scPTZ) seizures and neurotoxicity by motor impairment model in mice. The most active compoundN-(5-chlorobenzo[d]thiazol-2-yl)-2-(2,3-dioxoindolin-1-yl)acetamide (4a) has shown significant anticonvulsant activity against both MES and scPTZ screens and emerged as most effective anticonvulsant compound with median dose of 35.7 mg/kg (MES ED50), 88.15 mg/kg (scPTZ ED50) and toxic dose (TD50) was found to be > 500mg/kg. In silico studies including molecular docking study was carried to establish the molecular interaction of potent compound (4a) in both Na+ channel and GABAA receptors. The prediction of pharmacokinetic parameters and distance mapping of compounds were also performed to establish the drug likeness property.
- Akhtar, Md Jawaid,Debnath, Biplab,Grover, Gourav,Nath, Rajarshi,Pathania, Shelly,Shahar Yar, M.
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- CF3-, OCF3-, SCF3- AND SF5-CONTAINING ANTIBACTERIAL AGENTS
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The present invention generally relates to compounds as a new antibiotic to treat various infections, including infections caused by methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-intermediate and vancomycin-resistant S. aureus (VISA and VRSA respectively) vancomycin-resistant Enterococcus faecalis (VRE), and Clostridioides difficile. Pharmaceutical compositions and methods for treating those infection diseases are within the scope of this invention.
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Paragraph 0098-00100
(2020/11/03)
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- Ultrapotent Inhibitor of Clostridioides difficile Growth, Which Suppresses Recurrence in Vivo
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Clostridioides difficile is the leading cause of healthcare-associated infection in the U.S. and considered an urgent threat by the Centers for Disease Control and Prevention (CDC). Only two antibiotics, vancomycin and fidaxomicin, are FDA-approved for the treatment of C. difficile infection (CDI), but these therapies still suffer from high treatment failure and recurrence. Therefore, new chemical entities to treat CDI are needed. Trifluoromethylthio-containing N-(1,3,4-oxadiazol-2-yl)benzamides displayed very potent activities [sub-μg/mL minimum inhibitory concentration (MIC) values] against Gram-positive bacteria. Here, we report remarkable antibacterial activity enhancement via halogen substitutions, which afforded new anti-C. difficile agents with ultrapotent activities [MICs as low as 0.003 μg/mL (0.007 μM)] that surpassed the activity of vancomycin against C. difficile clinical isolates. The most promising compound in the series, HSGN-218, is nontoxic to mammalian colon cells and is gut-restrictive. In addition, HSGN-218 protected mice from CDI recurrence. Not only does this work provide a potential clinical lead for the development of C. difficile therapeutics but also highlights dramatic drug potency enhancement via halogen substitution.
- Naclerio, George A.,Abutaleb, Nader S.,Li, Daoyi,Seleem, Mohamed N.,Sintim, Herman O.
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p. 11934 - 11944
(2020/11/26)
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- Synthesis and amelioration of inflammatory paw edema by novel benzophenone appended oxadiazole derivatives by exhibiting cyclooxygenase-2 antagonist activity
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Ten new 2(4-hydroxy-3-benzoyl) benzamide-5-phenyl-1,3,4-oxadiazole derivatives (10a–j) were synthesized by coupling 3-benzoyl-4-hydroxybenzoic acid (5) with 2-amino-5-phenyl-1,3,4-oxadiazoles (9a–j). The structures of these compounds were confirmed by IR, 1H, 13C NMR, and mass spectra, and also by elemental analyses. The anti-inflammatory activity of the compounds 10a–j were investigated by screening them against human red blood cells (HRBC) in-vitro. The results reveal that among this series, compound 10j with hydroxy substituent, particularly at the ortho position of the phenyl ring attached to the 5th carbon atom of the oxadiazole ring possess significant membrane stabilizing activity in comparison with the control. Further, in-vivo chick chorioallantoic membrane (CAM) and rat corneal anti-angiogenesis assays were performed to assess the effect of compound 10j on endothelial cell migration. This confirmed that compound 10j inhibits the proliferation of endothelial cells. Anti-inflammatory studies detected the amelioration of carrageen induced rat hind paw edema. Further in-vivo and in-silico approaches revealed the inhibition of inflammatory marker enzyme cyclooxygenase-2 (Cox-2) and myleoperoxidase (MPO). The study reports that the compound 10j effectively act against the inflammatory mediated anti-angiogenic disorders which could be translated into a new drug in future.
- Puttaswamy, Naveen,Malojiao, Vikas H.,Mohammed, Yasser Hussein Eissa,Sherapura, Ankith,Prabhakar,Khanum, Shaukath Ara
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p. 1446 - 1455
(2018/05/22)
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- Synthesis and antimicrobial evaluation of novel 3-(arylideneamino)-3a,8a-dihydroxy-1,3,3a,8a-tetrahydroindeno[1,2-d]imidazole-2,8-diones and their 2-thioxo analogues
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The preparation of some novel 3-(arylideneamino)-3a,8a-dihydroxy-1,3,3a,8a-tetrahydroindeno[1,2-d]imidazole-2,8-diones 8(i–xiv) and 3-(arylideneamino)-3a,8a-dihydroxy-2-thioxo-1,3,3a,8a-tetrahydroindeno[1,2-d]imidazol-8(2H)-ones 9(i–xiv) have been reported through one-pot catalyst-free reaction of aldehydes, semicarbazide hydrochloride/thiosemicarbazide with ninhydrin. All the synthesized compounds have been screened for antimicrobial activity and some of them were observed to possess broad spectrum antibacterial potential as well as significant antagonistic potential against fungal pathogens.
- Saini, Yeshwinder,Khajuria, Rajni,Kaur, Ramneet,Kaul, Sanjana,Sharma, Tanwi,Gupta, Suruchi,Gupta, Vivek K.,Kant, Rajni,Kapoor, Kamal K.
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supporting information
p. 1159 - 1168
(2017/06/09)
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- Ultrasound-assisted synthesis of 2-amino-1,3,4-oxadiazoles through NBS-mediated oxidative cyclization of semicarbazones
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A ultrasound-assisted oxidative cyclization of semicarbazones using N-bromosuccinimide in the presence of sodium acetate was established providing efficient and rapid access to a variety of 2-amino-1,3,4-oxadiazoles. Moreover, the new synthetic protocol provides a simple procedure utilizing a safer oxidizing system that affords the target products in high regioselectivity, satisfactory yields, and elevated purities.
- Borsoi, Ana Flávia,Coldeira, Mateus Emanuel,Pissinate, Kenia,Macchi, Fernanda Souza,Basso, Luiz Augusto,Santos, Diógenes Santiago,Machado, Pablo
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supporting information
p. 1319 - 1325
(2017/07/12)
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- Design, synthesis, and biological activity of novel tetrahydropyrazolopyridone derivatives as FXa inhibitors with potent anticoagulant activity
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A series of novel tetrahydropyrazolopyridone derivatives containing 1,3,4-triazole, triazolylmethyl, and partially saturated heterocyclic moieties as P2 binding element was designed, synthesized, and evaluated in vitro for anticoagulant activity in human and rabbit plasma. All compounds showed moderate to significant potency, and compounds 15b, 15c, 20b, 20c, and 22b were further examined for their inhibitory activity against human FXa in vitro. While compounds 15c and 22b were tested for rat venous thrombosis in vivo. The most promising compound 15c, with an IC50 (FXa) value of 0.14?μM and 98% inhibition rate, warranted further investigation as an FXa inhibitor.
- Sun, Xiaoqing,Hong, Zexin,Liu, Moyi,Guo, Su,Yang, Di,Wang, Yong,Lan, Tian,Gao, Linyu,Qi, Hongxia,Gong, Ping,Liu, Yajing
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p. 2800 - 2810
(2017/04/18)
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- Oxidazol- gland glucoside compounds as inhibitors of TyrRS and its preparation and use
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Oxadiazole-adenosine compounds have a structural general formula as shown in the specification. The compounds have better inhibition and killing effects on various germs, part of compounds have higher bacteriostatic activity than positive control penicillin G, kamamycin and ketoconazole, and the compounds can be used for preparing anti-infective drugs. The invention discloses preparation methods of the oxadiazole-adenosine compounds and anti-pathogen microbial activity.
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Paragraph 0024; 0025
(2016/10/08)
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- Oxidazol- myo- glucoside compounds as inhibitors of TyrRS and its preparation and use
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A structural general formula of oxadiazole and inosine type compounds is as the following formal. The oxadiazole and inosine type compounds have a good role in restraining and killing multiple germs and a part of compounds are high in bacteriostatic activity compared with positive control penicillin G, kalamycin and ketoconazole and can be used for preparing anti-infective drugs. The invention discloses a preparation method and the pathogenic microorganism resistant activity.
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Paragraph 0024-0025
(2016/10/09)
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- Synthesis of 2-amino-1,3,4-oxadiazoles and 2-Amino-1,3,4-thiadiazoles via sequential condensation and I2-mediated oxidative C-O/C-S bond formation
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2-Amino-substituted 1,3,4-oxadiazoles and 1,3,4-thiadiazoles were synthesized via condensation of semicarbazide/thiosemicarbazide and the corresponding aldehydes followed by I2-mediated oxidative C-O/C-S bond formation. This transition-metal-free sequential synthesis process is compatible with aromatic, aliphatic, and cinnamic aldehydes, providing facile access to a variety of diazole derivatives bearing a 2-amino substituent in an efficient and scalable fashion.
- Niu, Pengfei,Kang, Jinfeng,Tian, Xianhai,Song, Lina,Liu, Hongxu,Wu, Jie,Yu, Wenquan,Chang, Junbiao
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p. 1018 - 1024
(2015/01/30)
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- Synthesis and antitubercular activity of 2-(1H-pyrrol-1-Yl)-5- substituted-1,3,4-oxadiazoles
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A series of 2-(1H-pyrrol-1-yl)-5-substituted-1,3,4-oxadiazole derivatives were prepared and evaluated for their antitubercular activity. These derivatives were synthesized by the reaction of 5-substituted-1,3,4-oxadiazol-2-amines (4a-j) with 2,5- dimethoxytetrahydrofuran in dried acetic acid. Structures of the newly synthesized compounds were confirmed on the basis of physico-chemical and spectral data. All the synthesized compounds were screened for their antitubercular activity using microplate almar blue assay (MABA) method. Compounds have shown moderate to good antitubercular activity against M. tuberculosis H37Rv microorganism.
- Joshi, Shrinivas D.,Dixit, Sheshagiri R.,More, Uttam A.,Kulkarni, Venkatrao H.
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p. 137 - 140
(2019/01/21)
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- Novel limonene and citral based 2,5-disubstituted-1,3,4-oxadiazoles: A natural product coupled approach to semicarbazones for antiepileptic activity
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Two novel series of N4-(5-(2/3/4-substituted-phenyl)-1,3,4- oxadiazol-2-yl)-N1-(2-methyl-5-(prop-1-en-2-yl)cyclohex-2-enylidene) semicarbazide and N4-(5-(2/3/4-substituted-phenyl)-1,3,4-oxadiazol-2- yl)-N1-(3,7-dimethylocta-3,6-dienylidene)-semicarbazide were synthesized to meet structural prerequisite indispensable for anticonvulsant activity. The anticonvulsant activities of the compounds were investigated using maximal electroshock seizure (MES), subcutaneous pentylenetrtrazole (scPTZ) and subcutaneous strychnine (scSTY) models. The rotorod test was conducted to evaluate neurotoxicity. Some of the selected active compounds were subjected to GABA assay to confirm their mode of action. The outcome of the present investigations proved that the four binding sites pharmacophore model is vital for anticonvulsant activity. The efforts were also made to establish structure-activity relationships among test compounds.
- Rajak, Harish,Singh Thakur, Bhupendra,Singh, Avineesh,Raghuvanshi, Kamlesh,Sah, Anil Kumar,Veerasamy, Ravichandran,Sharma, Prabodh Chander,Singh Pawar, Rajesh,Kharya, Murli Dhar
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p. 864 - 868
(2013/02/25)
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- Oxadiazolo pyrrolidine carboxamides as enoyl-ACP reductase inhibitors: Design, synthesis and antitubercular activity screening
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Pyrrolidine carboxamides have been recognized as potent direct enoyl-acyl carrier protein reductase inhibitors. In our study, the search for new pyrrolidine carboxamides incorporated with various heterocyclic moieties, possessing antitubercular activities is been done. A series of oxadiazolyl pyrrolidine carboxamides (2a-e) were synthesized by reacting pyrrolidine carboxylic acid and oxadiazole amines using HBTU as amide forming agent. The purity of the synthesized compounds was confirmed by physical characterization like melting point and thin layer chromatography. The functional group identification was done based on spectral characterization utilizing, FT-IR, 1H NMR, 13C NMR, mass spectral data and elemental analysis. Invitro antitubercular screening was performed by alamar blue assay method on mycobacterium tuberculosis H37Rv.
- Sonia, George,Ravi, Thengungal Kochupappy
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p. 3428 - 3433
(2013/07/11)
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- Synthesis and antiviral activity of new substituted methyl [2-(arylmethylene-hydrazino)-4-oxo-thiazolidin-5-ylidene]acetates
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A series of new methyl [2-(arylmethylene-hydrazono)-4-oxo-thiazolidin-5- ylidene]acetates (5a-o) were synthesized via cyclocondensation of thiosemicarbazones (3a-o) with dimethyl but-2-ynedioate (4) in good yields under solvent-free conditions. The environmentally friendly solvent-free protocol overcomes the limitations associated with the customary protracted solution phase synthesis and afforded the title compounds in a few minutes. Compounds 5b-i and 5h-o were evaluated for their antiviral activity against the replication activity of HIV-1 and HIV-2 in MT-4 using the MTT assay. The same compounds were also evaluated in vitro for their selective antiviral activity against hepatitis C virus (HCV) in the Huh 5-2 replicon system (type 1b, Con1 strain).
- Saeed, Aamer,Al-Masoudi, Najim A.,Latif, Muhammad
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p. 618 - 625
(2013/09/02)
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- Cyclization of the semicarbazones to 1,3,4-oxadiazole derivatives using ceric ammonium nitrate as oxidant
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Cyclization of the semicarbazones to 1,3,4-oxadiazole using ceric ammonium nitrate as oxidant was studied. 2-Imino-1,3,4-oxadiazolines can be produced from semicarbazones, which undergo thermolysis to amides. Benzoic acid benzylidene hydrazide can also be cyclized to 2-methoxy-2-phenyl-1,3,4-oxadiazole in the presence of ceric ammonium nitrate and methanol.
- Vahedi,Lari,Bavand,Ameri
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experimental part
p. 288 - 290
(2012/08/08)
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- Synthesis and in vitro antitumor activity of 1,3,4-oxadiazole derivatives based on benzisoselenazolone
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A series of novel 1,3,4-oxadiazole derivatives based on benzisoselenazolone has been prepared and tested for antiproliferative activity in vitro against the cells of human cancer cell lines: SSMC-7721 (human liver cancer cell), MCF-7 (human breast cancer cell) and A549 (human lung cancer cell). All the compounds obtained exhibited antiproliferative activity and showed selective cytotoxicity against different cancer cells. Compounds 7d and 7i showed significant antiproliferative activities against MCF-7 cells, with IC50 values of 1.07 and 1.76/μM respectively. Compound 7d were found to be the most potent compound against SSMC-7721 cells, with IC50 values 4.46/μM.
- Luo, Zhen-Hua,He, Shuang-Yan,Chen, Bao-Quan,Shi, Yan-Ping,Liu, Yu-Ming,Li, Cai-Wen,Wang, Qiu-Sheng
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experimental part
p. 887 - 891
(2012/08/14)
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- Microwave assisted synthesis and characterization of semicarbazones
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An efficient and simple microwave assisted procedure has been developed for conversion of substituted aryl aldehyde to corresponding semicarbazone by reaction with semicarbazide hydrochloride in presence of sodium acetate. The synthesized semicarbazones have been characterized by physico-chemical and spectral data.
- Jadon, Sudha,Khedr, Abdalla M.,Kumar, Sanjeev,Yadav, Sneha,Kumar, Vipin,Gupta, Kishan C.
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experimental part
p. 4209 - 4211
(2012/01/04)
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- 2,5-Disubstituted-1,3,4-oxadiazoles/thiadiazole as surface recognition moiety: Design and synthesis of novel hydroxamic acid based histone deacetylase inhibitors
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The enzymatic inhibition of histone deacetylase activity has come out as a novel and effectual means for the treatment of cancer. Two novel series of 2-[5-(4-substitutedphenyl)-[1,3,4]-oxadiazol/thiadiazol-2-ylamino] -pyrimidine-5-carboxylic acid (tetrahydro-pyran-2-yloxy)-amides were designed and synthesized as novel hydroxamic acid based histone deacetylase inhibitors. The antiproliferative activities of the compounds were investigated in vitro using histone deacetylase inhibitory assay and MTT assay. The synthesized compounds were also tested for antitumor activity against Ehrlich ascites carcinoma cells in Swiss albino mice. The efforts were also made to establish structure-activity relationships among synthesized compounds. The results of the present studying indicates 2,5-disubstituted 1,3,4-oxadiazole/thiadiazole as promising surface recognition moiety for development of newer hydroxamic acid based histone deacetylase inhibitor.
- Rajak, Harish,Agarawal, Avantika,Parmar, Poonam,Thakur, Bhupendra Singh,Veerasamy, Ravichandran,Sharma, Prabodh Chander,Kharya, Murli Dhar
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supporting information; scheme or table
p. 5735 - 5738
(2011/10/09)
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- Synthesis, anticonvulsant and neurotoxic activity of some new 2,5-disubstituted-1,3,4-oxadiazoles
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Two novel series 2a-2d (2Z)-N-[5-(4-substituted) phenyl-1,3,4-oxadiazol-2- yl]-2-[(2Z)-3,7-dimethylocta- 2,6-dien-1-ylidene]hydrazinecarboxamide and 1a-1d 5-(4-substituted)phenyl-N-[(1Z,2Z)-3,7-dimethylocta-2,6- dien-1-ylidene]-1,3,4- oxadiazol-2-amine have been synthesized and screened for their anticonvulsant and neurotoxic activity. After i.p. injection to mice at doses of 30, 100 and 300 mg/kg body weight 2,5-disubstituted-1,3,4- oxadiazole analogues were examined in the maximal electroshock induced seizures (MES) and subcutaneous metrazole (ScMET) induced seizure models in mice. Amongst all the compounds, 1a-1d and 2a-2d, one compound 1a exhibited activity at 100 mg/kg body weight at 0.5 and 4 h in ScMET, respectively. Compound 2b showed anticonvulsant activity at 100 mg/kg without activity in ScMET and neurotoxicity. The neurotoxicity was assessed by rotorod method, and all compounds (except 1a) were found to be safe at maximum administered dose. Springer Science+Business Media, LLC 2010.
- Jain, Neha,Kashaw, Sushil K.,Agrawal,Gupta, Anjali,Soni, Abhishek
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experimental part
p. 1696 - 1703
(2012/06/16)
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- Design and synthesis of some novel 3-[5-(4-substituted) phenyl- 1,3,4-oxadiazole-2yl]-2-phenylquinazoline-4(3H)-ones as possible anticonvulsant agent
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A novel series 7(a-f) 3-[5-(4-substituted) phenyl- 1,3,4-oxadiazole-2yl]-2 phenylquinazoline-4(3H)-ones have been synthesized and screened for its anticonvulsant and neurotoxic activity. After i.p. injection to mice at doses of 30, 100, and 300 mg/kg body weight 2,3-disubstitutedquinazolin- 4(3H)-ones were examined in the maximal electroshock induced seizures (MES) and subcutaneous pentylenetetrazole (scPTZ) induced seizure models in mice. Spectroscopic data were consistent with the structure of newly synthesized compounds. The neurotoxicity was assessed using the rotorod method. In the prepared series, 7a was found to be active in the MES screen at 0.5 h, whereas 7f showed anticonvulsant activity at both 0.5 and 4 h. Springer Science+Business Media, LLC 2010.
- Gupta, Anjali,Kashaw, Sushil K.,Jain, Neha,Rajak, Harish,Soni, Abhishek,Stables
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experimental part
p. 1638 - 1642
(2012/06/05)
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- Anticonvulsant and sedative-hypnotic activity of some novel 3-[5-(4-substituted) phenyl-1,3,4-oxadiazole-2yl]-2-styrylquinazoline-4(3H)-ones
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A few novel 3-[5-(4-substituted) phenyl-1,3,4-oxadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones were synthesized and evaluated for anticonvulsant, neurotoxicity, sedative-hypnotic, and phenobarbitone-induced hypnosis potentiation test. After i.p. injection to mice at doses of 30, 100, and 300 mg/kg body weight derivatives were examined in the maximal electroshock-induced seizures (MES) and subcutaneous pentylenetetrazole (scPTZ)-induced seizure models in mice. Spectroscopic data were consistence with the newly synthesized compounds. The neurotoxicity was assessed using the Rotorod method. Out of 15 compounds only 7e and 7o showed anticonvulsant activity at various doses in one or more test models. All except 7d, 7m, and 7n exhibited significant sedative-hypnotic activity via actophotometer screen. Central nervous system (CNS)-depressant activity screened with the help of the forced swim method resulted into some potent compounds. No percentage increase in the sleeping time was observed in any of the synthesized compounds evaluated by the phenobarbitone-induced hypnosis potentiation test. On the basis of experimental data, it can be concluded that synthesized compounds possessed relatively better sedative-hypnotic and CNS-depressant activities.
- Kashaw, Sushil K.,Gupta, Vivek,Kashaw, Varsha,Mishra,Stables,Jain
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experimental part
p. 250 - 261
(2011/01/12)
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- Effect of semicarbazones on endogenous protein hydrolysis in liver homogenate
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Semicarbazones of substituted benzaldehydes were synthesized and their effect on endogenous protein hydrolysis in liver homogenate was studied. It was found that p-nitrobenzaldehyde semicarbazone exerted maximum effect.
- Raghav,Kaur, Ravinder,Singh, Mamta,Suman,Priyanka
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experimental part
p. 7097 - 7101
(2012/07/17)
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- Synthesis and antimicrobial activity of some new 3-[5-(4-substituted) phenyl-1,3,4-oxadiazole-2yl]-2- styrylquinazoline-4(3H)-ones
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Several 3-[5-(4-substituted)phenyl-1,3,4-oxadiazole-2-yl]-2-styryl quinazoline-4(3H)-one were synthesized and screened for antibacterial activity against Staphylococcus aureus , Bacillus subtilis, Pseudomonas aeruginosa, and Escherichia coli and antifungal activity against Aspergillus niger and Fusariumoxysporum by the serial dilution technique. Compounds were prepared by reacting corresponding 2-methtyl quinazolinone and 4-subustituted benzaldehydes in glacial acetic acid. Physicochemical and spectral data were consistent with newly synthesized compounds. The prepared compounds were compared with previously synthesized 2-methyl-3-[5-(4-substituted)phenyl-1,3,4-oxadiazole-2- yl]-quinazoline-4(3H)-ones for antimicrobial activity. The present study revealed that styryl moiety at the second position of 4(3H) quinazolinone marginally increased the biological activity and exhibited better antibacterial than antifungal activities.
- Gupta, Vivek,Kashaw, Sushil K.,Jatav, Varsha,Mishra, Pradeep
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p. 205 - 211
(2008/12/22)
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- Basic alumina as an efficient catalyst for preparation of semicarbazones in solvent free conditions
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An efficient and simple procedure for conversion of different classes of aldehydes and ketones into the corresponding semicarbazones with semicarbazide hydrochloride using basic alumina is studied.
- Kiasat, Ali Reza,Kazemi, Foad,Mehrjardi, Mehdi Fallah
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p. 1337 - 1339
(2008/03/13)
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- Solventless rapid synthesis of oxime, semicarbazone, and phenylhydrazone derivatives from carbonyl compounds under microwave conditions
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A rapid and efficient method for the synthesis of oximes, semicarbazones, and phenylhydrazones has been reported under solventless conditions using microwave irradiation. CSIRO 2005.
- Kamakshi,Reddy, Boreddy S. R.
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p. 603 - 606
(2007/10/03)
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- Reactions of trichloromethylarenes with hydrazine derivatives. Synthesis of 2,5-disubstituted 1,3,4-oxadiazoles and 1,3,4-thiadiazoles
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The effect of the solvent on the course of the reaction between trichloromethylarenes and thioacylhydrazines or acylhydrazines has been considered. In alcohols as solvents, alkyl arenecarboxylates form as a result of alcoholysis, while 2,5-disubstituted 1,3,4-thiadiazoles (1,3,4-oxadiazoles) form as minor products. In pyridine solutions, the major or sole products are those of reductive condensation, i.e., the corresponding N-substituted hydrazones of arenecarbaldehydes. 1,3,4-Thiadiazole or 1,3,4-oxadiazole derivatives are obtained in good yield when the reaction is carried out in a pyridine - alkanol mixture.
- Poddubnyi,Belen'kii,Krayushkin
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p. 1185 - 1188
(2007/10/03)
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- Coordination Compounds of Tantalum(V)
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Ta(OPri)4(SB), Ta(OPri)3(SB)2 and Ta(OPRi)2(SB)3 types of complexes of tantalum with aldimines (SBH) of the type o-OHC6H4CH:NC6H4CH3-o, o-OHC6H4CH:NC4H9-n, C6H5CH:NNHCONH2 and C6H5CH:NNHCSNH2 have been synthesized by the reactions of tantalum pentaisopropoxide.The aldimines were obtained by the condensation of salicylaldehyde with o-methylaniline and n-butylamine and of benzaldehyde with semicarbazide hydrochloride and thiosemicarbazide.The complexes have been fully characterised by their analytical data, conductance, magnetic and molecular weight measurement and IR, electronic and PMR data.
- Mookerjee, M. N.,Singh, R. V.,Tandon, J. P.
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p. 521 - 522
(2007/10/02)
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- Polymer-supported Periodate and Iodate as Oxidizing Agents
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The periodate forms of some commercial macroporous anion-exchange resins can be used in either protic or aprotic solvents to oxidize various quinols, catechols, and glycols and also triphenylphosphine, hydrazobenzene, and benzohydroxamic acid.The reagents in methanol oxidize thioethers.Polymer-supported iodate also oxidizes quinols and catechols.
- Harrison, Charles R.,Hodge, Philip
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p. 509 - 511
(2007/10/02)
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